CN103338746A - Composition containing polyunsaturated fatty acid - Google Patents
Composition containing polyunsaturated fatty acid Download PDFInfo
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- CN103338746A CN103338746A CN2012800064407A CN201280006440A CN103338746A CN 103338746 A CN103338746 A CN 103338746A CN 2012800064407 A CN2012800064407 A CN 2012800064407A CN 201280006440 A CN201280006440 A CN 201280006440A CN 103338746 A CN103338746 A CN 103338746A
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/201—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having one or two double bonds, e.g. oleic, linoleic acids
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
- A61K31/355—Tocopherols, e.g. vitamin E
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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Abstract
The purpose of the present invention is to provide a composition for external applications, in which the long-term stability of a polyunsaturated fatty acid is further increased. The present invention provides a composition as mentioned below. In the composition, the long-term stability of a polyunsaturated fatty acid is improved. A composition comprising components (A) and (B) as mentioned below, wherein the component (B) is dispersed in a continuous phase containing the component (A): (A) at least one component selected from the group consisting of tocopherol and phytic acid; and (B) a liposome containing a polyunsaturated fatty acid or a derivative thereof.
Description
Technical field
The present invention relates to contain the compositions (preferred topical composition) of polyunsaturated fatty acid.
Background technology
Polyunsaturated fatty acid is blended in the topical composition (for example, cosmetics and topical drug) that expection has skin whitening effect etc.Yet known polyunsaturated fatty acid has poor ageing stability, and the content of polyunsaturated fatty acid of compositions reduced along with the time.In addition, the compositions with the polyunsaturated fatty acid fusion can be coloured or send poor abnormal smells from the patient.Particularly in Japan, requirements such as law, rules contain polyunsaturated fatty acid as the topical composition of effective ingredient after producing based on concrete amount stably keep 90% or above polyunsaturated fatty acid reach 3 years.Therefore, needed to develop effective stabilization technology.For example, following technology has been proposed to improve the ageing stability of polyunsaturated fatty acid: the technology (PTL1) of mixing eugenol, isoeugenol, vitamin K etc.; The technology (PTL2 to PTL4) of mixing the polyunsaturated fatty acid of esterification; Production comprises the aerocolloidal technology (PTL5) of nitrogen and the content of the lipid that contains highly unsaturated fatty acid; Produce the technology of Emulsion, wherein polyunsaturated fatty acid is mixed (PTL6) with dispersant such as the vitamin E of specified quantitative.
The quoted passage tabulation
Patent documentation
PTL1：JP63-72654A
PTL2：JP2007-126438A
PTL3：JP2007-269683A
PTL4：JP2007-269684A
PTL5：JP8-81326A
PTL6：JP2010-502733A
Summary of the invention
Technical problem
The purpose of this invention is to provide and comprise the topical composition that polyunsaturated fatty acid has higher ageing stability.
The solution of problem
Result as In view of the foregoing broad research, the inventor is surprised to find, can be by the polyunsaturated fatty acid or derivatives thereof be attached in the liposome, liposome is dispersed in the disperse medium (continuous phase), and will be selected from that at least one member in the group of being made up of tocopherol and phytic acid joins continuous phase and the compositions that obtains to comprise the polyunsaturated fatty acid with excellent ageing stability.The inventor is further improved to realize the present invention.
More specifically, the present invention includes compositions etc., it is described in the following project:
1. 1 kinds of compositionss of project, its comprise below shown in component (A) and component (B), described component (B) is dispersed in the continuous phase that contains described component (A):
(A) be selected from least one member in the group of being formed by tocopherol and phytic acid; With
(B) contain the liposome of polyunsaturated fatty acid or derivatives thereof.
Project 2. is according to the compositions of project 1, and wherein said tocopherol is at least one member who is selected from the group of being made up of alpha-tocopherol, betatocopherol, Gamma-Tocopherol, Delta-Tocopherol, dl-alpha-tocopherol acetate, dl-alpha-tocopherol and d-alpha-tocopherol acetate.
Project 3-1. is according to the compositions of project 1 or 2, and wherein said polyunsaturated fatty acid has 18 to 22 carbon atoms.
Project 3-2. is according to each compositions in the project 1 to 3-1, and wherein said polyunsaturated fatty acid has 2 to 6 two keys.
Project 4. is according to each compositions in the project 1 to 3-2, and wherein said continuous phase contains phytic acid at least.
Project 5. is according to each compositions in the project 1 to 4, and wherein said continuous phase contains Delta-Tocopherol at least.
Project 6. is according to each compositions in the project 1 to 5, and wherein said continuous phase also contains at least one member who is selected from the group of being made up of L-cystine and L-threonine.
Project 7. is according to each compositions in the project 1 to 6, and wherein said liposome also contains at least one member who is selected from the group of being made up of tocopherol and phytic acid.
Project 8. is according to each compositions in the project 1 to 7, and described compositions is the compositions for external application.
The method of a project A-1. skin whitening, described method comprise and will be administered to the step of skin according to each compositions in the project 1 to 8.
Treatment or the beauty method of a project A-2. skin whitening, described method comprise and will be administered to the step of skin according to each compositions in the project 1 to 8.
Item B-1. is according to each compositions in the project 1 to 8, and described compositions is used for the skin whitening treatment.
Project C-1. is used for the purposes of the medicine of skin whitening treatment in production according to each compositions in the project 1 to 8.
The beneficial effect of the invention
In topical composition of the present invention, the polyunsaturated fatty acid that is included in the liposome has high ageing stability.This can effectively utilize skin whitening effect of polyunsaturated fatty acid etc.
Embodiment is described
Compositions of the present invention comprises following component (A) and (B):
(A) be selected from least one member in the group of being formed by tocopherol and phytic acid; With
(B) contain the liposome of polyunsaturated fatty acid or derivatives thereof.
In compositions of the present invention, component (B) is dispersed in the disperse medium (continuous phase) that comprises component (A).That is, compositions of the present invention is disperse system, and wherein component (A) is comprised in the disperse medium, and component (B) is dispersate.
In other words, compositions of the present invention comprises said components (A) and (B), and wherein said component (B) is dispersed in the disperse medium (continuous phase) that comprises component (A).
In compositions of the present invention, component (A) is included therein in the continuous phase of having disperseed liposome at least.In addition, component (A) preferably not only is comprised in the continuous phase, but also is comprised in the liposome.The component (A) that is comprised in the liposome more preferably is tocopherol.Component (A) can be attached in the liposome, by itself and phospholipid, polyunsaturated fatty acid etc. are used in combination, as the initiation material for the preparation of liposome.
In being comprised in continuous phase or when being comprised in the liposome, the tocopherol that uses among the present invention is preferably selected from the group of being made up of alpha-tocopherol, betatocopherol, Gamma-Tocopherol, Delta-Tocopherol, dl-alpha-tocopherol acetate, dl-alpha-tocopherol and d-alpha-tocopherol acetate.These tocopherols can be individually or with two or more being used in combination.More preferably, use as in alpha-tocopherol, betatocopherol, Gamma-Tocopherol and the Delta-Tocopherol of naturally occurring tocopherol one or more.Especially, Delta-Tocopherol is most preferred in these tocopherols, because can obtain high effect.
Based on the gross weight of compositions of the present invention, tocopherol content is preferably about 0.005 to 0.5 quality %, and about 0.01 to 0.1 quality % more preferably.Tocopherol content more than 0.005 quality %, effect of the present invention can further be represented.In addition, the tocopherol content below 0.5 quality % can obtain described effect (that is, when tocopherol content during greater than 0.5 quality %, though the content height of tocopherol, the effect that obtains may be low) effectively.
In the present invention, liposome contains polyunsaturated fatty acid.The polyunsaturated fatty acid of Shi Yonging preferably has the individual carbon atom in 18 to 22 (18,19,20,21 or 22) in the present invention.The polyunsaturated fatty acid that further preferably has the individual pair of key in 2 to 6 (2,3,4,5 or 6).The polyunsaturated fatty acid that more preferably has 18 to 22 carbon atoms and 2 to 6 two keys.Its instantiation comprises linoleic acid, alpha-linolenic acid, gamma-Linolenic acid, dihomo-gamma-linolenic acid, arachidonic acid, eicosapentaenoic acid, docosahexenoic acid etc.In addition, the salt of polyunsaturated fatty acid also can use in the present invention.The example comprises the polyunsaturated fatty acid slaine, as polyunsaturated fatty acid sodium salt and polyunsaturated fatty acid potassium salt; The polyunsaturated fatty acid amino acid salts is as polyunsaturated fatty acid arginine salt and polyunsaturated fatty acid lysinate; The polyunsaturated fatty acid amine salt is as polyunsaturated fatty acid triethanolamine salt and polyunsaturated fatty acid monoethanolamine salt etc.The instantiation of the salt of polyunsaturated fatty acid comprises linoleic acid sodium salt, alpha-linolenic acid potassium salt etc.; Linoleic acid arginine salt, alpha-linolenic acid lysinate etc.; With trietbanolamine linoleate salt, alpha-linolenic acid monoethanolamine salt etc.
In addition, in the present invention, also can use the polyunsaturated fatty acid derivant to replace or be additional to polyunsaturated fatty acid.The preferred embodiment of described derivant comprises monoesters and the diester of polyunsaturated fatty acid, as Ethyl linoleate, Alpha-ethyl linolenate, Sunsoft 8090, alpha-linolenic acid monoglyceride, linoleic acid diglyceride and alpha-linolenic acid diglyceride.
Particularly preferably be linoleic acid, alpha-linolenic acid, Ethyl linoleate, Alpha-ethyl linolenate, Sunsoft 8090 and alpha-linolenic acid monoglyceride in these; Linoleic acid is most preferred in these.The polyunsaturated fatty acid or derivatives thereof can be individually or is two or morely used in combination.Gross weight based on the present composition, the content of such polyunsaturated fatty acid or derivatives thereof is preferably 0.01 to 1 quality %, 0.05 to 0.5 quality % more preferably, 0.08 to 0.2 quality % more preferably also, and 0.09 to 0.11 quality % more preferably.When the content of polyunsaturated fatty acid or derivatives thereof is 0.01 quality % when above, compositions that can the application of the invention more effectively obtains whitening effect.On the contrary, when this content is 1 quality % when following, have such risk still less, namely said composition will produce disagreeable abnormal smells from the patient or in time and the generation variable color and the effect that can't obtain to mate content of polyunsaturated fatty acid.
The liposome of Shi Yonging preferably contains lecithin as component (particularly membrane component) in the present invention.The example of lecithin comprises soybean lecithin, Semen Maydis lecithin, Oleum Gossypii semen lecithin, Ovum Gallus domesticus Flavus lecithin, albumen lecithin etc.In addition, also can use the lecithin derivant to replace or be additional to lecithin.The example of lecithin derivant comprises hydrolecithin and by Polyethylene Glycol, aminoglycan etc. being incorporated into the chemical compound that obtains in the phospholipid of above-mentioned lecithin.In these, soybean lecithin, Ovum Gallus domesticus Flavus lecithin, hydrogenated soy phosphatidyl choline and hydrogenated yolk lecithin are preferred, and particularly preferably are soybean lecithin and Ovum Gallus domesticus Flavus lecithin.In addition, also can preferably use the lecithin that is present in the purification of phospholipid (as phosphatidylcholine, Phosphatidylserine, PHOSPHATIDYL ETHANOLAMINE, phosphatidylinositols, phosphatidyl glycerol and sphingomyelins) the purity acquisition in the lecithin by increase.These lecithin or lecithin derivant can be individually or are two or morely used in combination.
For example, can produce compositions of the present invention by preparation liposome dispersion, the liposome (component (B)) that wherein will contain the polyunsaturated fatty acid or derivatives thereof is dispersed in the liquid dispersion medium, and component (A) is added in the continuous phase of liposome dispersion.Water usually can be as the disperse medium of liposome dispersion.When the disperse medium of liposome dispersion is water, and when component (A) is slightly water-soluble material (tocopherol), component (A) can be dispersed in the water or is dissolved in the water with surfactant.In the present invention, component (A) is preferably dissolved in the disperse medium.
The method for preparing the liposome dispersion is not particularly limited, and can use standard method.The example of such method is as follows:
(1) a kind of method for preparing liposome in the following manner: phospholipid, unsaturated fatty acid or derivatives thereof and other component that will comprise are mixed equably, and with the mixture that obtains and the aqueous solution hydration that contains pH regulator agent, polyhydric alcohol, sugar etc.;
(2) a kind of method for preparing liposome in the following manner: with phospholipid, polyunsaturated fatty acid or derivatives thereof and other components dissolved that will comprise in alcohol, polyhydric alcohol etc., and with the mixture that obtains and the aqueous solution hydration that contains pH regulator agent, polyhydric alcohol, sugar etc.;
(3) a kind of method for preparing liposome in the following manner: use ultrasound wave, French press, homogenizer etc. in water, to form phospholipid, polyunsaturated fatty acid or derivatives thereof and the complex of other component that will comprise; With
(4) a kind of method for preparing liposome in the following manner: in ethanol, mix and dissolving phospholipid, polyunsaturated fatty acid or derivatives thereof and other component that will comprise, and the alcoholic solution that obtains is added in the potassium chloride solution, then remove ethanol.
The liposome dispersion can contain polymer, protein and hydrolyzate, mucopolysaccharide etc.That is, by using polymer, protein, protein hydrolysate, mucopolysaccharide etc. can produce the liposome dispersion as raw material.The example of the polymer in the liposome dispersion to be mixed includes, but not limited to CVP Carbopol ETD2050, xanthan gum, sodium alginate etc.Wherein preferably CVP Carbopol ETD2050 and xanthan gum, and particularly preferably be xanthan gum.Based on whole liposome dispersions, these polymer can use or two or more use in combination individually.Polymer content is, but is not limited to 0.001 to 20 quality %, preferred 0.01 to 10 quality %, and preferred especially 0.05 to 5 quality % especially.The example of protein and hydrolyzate thereof comprises collagen protein, elastin laminin, keratin, casein and other protein; The hydrolyzate of these protein; The salt of described hydrolyzate; The ester of described hydrolyzate; Handle product with the enzyme of described hydrolyzate.Based on whole liposome dispersions, the content of protein and hydrolyzate thereof is, but is not limited to especially, 0.001 to 5 quality %, and be preferably 0.01 to 1 quality %.The example of mucopolysaccharide comprises chondroitin sulfate, hyaluronic acid, dermatan sulfate (dermatan sulfate), Heparan sulfate, mucoitinsulfuric acid, heparin and derivant thereof, and salt; Wherein chondroitin sulfate, hyaluronic acid and sodium salt thereof are particularly preferred.Based on whole liposome dispersions, mucopolysaccharide content is, but is not limited to especially, 0.0005 to 5 quality %, and be preferably 0.001 to 1 quality %.
Can be by preparation compositions of the present invention in the continuous phase that component (A) is attached to the liposome dispersion, as mentioned above.In addition, in the scope of not damaging effect of the present invention, also the component that is different from component (A) can be attached in the continuous phase of liposome dispersion.
For example, when the disperse medium of liposome dispersion is water, and when component (A) is slightly water-soluble material (tocopherol), as mentioned above, can further add surfactant and it is dissolved in the continuous phase (be water, it is as disperse medium) of dispersion.
The preferred embodiment of surfactant comprises non-ionic surface active agent, as polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated Oleum Ricini and polyglyceryl fatty acid ester surfactant.Wherein, preferably six fatty acid glycerides and ten fatty acid glycerides are as six polyglycereol monolaurates (hexaglycerol monolaurate), six polyglycereol list myristinates (hexaglycerol monomyristate), six polyglycereol monostearates (hexaglycerol monostearate), six polyglycereol monoleates (hexaglycerol monooleate), ten polyglycereol monolaurates (decaglycerol monolaurate), ten polyglycereol monoleates (decaglycerol monooleate), ten polyglycereol list linoleates (decaglycerol monolinoleate) and ten polyglycereol list isostearates (decaglycerol monoisostearate).These surfactants can be individually or are two or morely used in combination.
In addition, can in the continuous phase of liposome dispersion, contain (preferred dissolution) L-cystine and/or L-threonine.It is preferred using L-cystine and L-threonine " contain the compositions of component (A) and component (B), component (B) is dispersed in the continuous phase that contains component (A) ", because they can further increase the stability of polyunsaturated fatty acid.
In the present invention, L-cystine and L-threonine can use individually or in combination; Yet preferred compositions ground uses them, because can obtain higher effect.Based on the gross weight of the present composition, the amount of L-cystine and L-threonine is preferably 0.0001 to 0.2 quality %, 0.0005 to 0.1 quality % more preferably, and even 0.001 to 0.06 quality % more preferably.
When the present invention was used as topical composition, also can use usually can be for the production of the component (being comprised in the continuous phase of liposome dispersion) of topical composition.The example of such component comprises wetting agent, water-soluble polymer, oil ingredient, coloring agent, antioxidant, sequestering agent, antiseptic, pH regulator agent, cold-producing medium, aromatic, UV absorption and scattering diluent, antioxidant, medicinal property, etc.
The example of wetting agent comprises polyhydric alcohol, as propylene glycol, 1,3 butylene glycol and glycerol; High molecular weight polysaccharide, plant extract, microbial metabolic products etc.These wetting agent can be individually or are two or morely used in combination.
The example of water-soluble polymer comprises cellulose derivative, CVP Carbopol ETD2050, xanthan gum, polyvinyl pyrrolidone, (acrylate/steareth-20 itaconate) copolymer, (acrylate/C10-30 alkyl acrylate) cross linked polymer (crosspolymer), (acrylate/palmeth-25 acrylate) copolymer, (acrylate/ceteth-20 itaconate) copolymer, (acrylate/C12-22 alkylmethacrylate) copolymer, (acrylate/beheneth-25 methacrylate) copolymer, (acrylate/steareth-20 methacrylate) cross linked polymer, agar, pectin, gellan gum (gellan gum), gelatin, clay mineral etc.These water-soluble polymers can be individually or are two or morely used in combination.
The example of oil ingredient comprises animal oil, vegetable oil, mineral oil, hydrocarbon ils, ester oil, wax, higher alcohol, higher fatty acids, silicone oil and derivant thereof, vaseline, quintessence oil etc.These oil ingredients can be individually or are two or morely used in combination.
In addition, when the present invention was used as topical composition, in the scope of not damaging effect of the present invention, the component that can be included in usually in the liposome also can be used in the preparation of liposome.The example comprises antioxidant, as ascorbic acid; Organic acid is as lactic acid and citric acid; Lipid is as phosphatidyl glycerol and PHOSPHATIDYL ETHANOLAMINE; Natural polymer is as chitosan, fucoidan and hyaluronic acid; Synthetic polymer is as Polyethylene Glycol and CVP Carbopol ETD2050; Sugar, as trehalose, lactulose and maltose alcohol; Polyhydric alcohol is as glycerol etc.
Compositions of the present invention is preferably used as topical composition (will be applied to the compositions of skin).The example of topical composition comprises pharmaceutical composition, accurate pharmaceutical composition and cosmetic composition.Particularly preferably being with the form of medicine, accurate medicine or cosmetics uses compositions of the present invention as the topical composition with skin whitening effect (that is the skin whitening composition of external).The dosage form of compositions is not particularly limited.The example of dosage form comprises facial cream, paste, ointment, cream, gel, lotion, emulsion, essence, facial lotion, spray etc.
When compositions of the present invention was used as topical composition, the target of using was not particularly limited, but preferably wants the people of skin whitening.
The present invention also comprises the method (skin whitening method) for skin whitening, and described method comprises the step that compositions of the present invention is administered to target skin.For example, the method can be used for treatment and cosmetic purpose.That is, the skin whitening method comprises treatment and the cosmetic method for skin whitening.More specifically, the method of whitening of mentioning herein is passable, for example, be used for the treatment of speckle (spots), obscure (dullness), chloasma (melasma), postinflammatory hyperpigmentation (post-inflammatory hyperpigmentation) etc., or be used for the cosmetic purpose.Application target and application dosage are as mentioned above.
Embodiment
Embodiments of the invention are described below, and still, the present invention is not limited to following examples." % " expression " quality % ", unless otherwise prescribed.
The ageing stability test of polyunsaturated fatty acid
Prepare the dispersion that contains linoleic liposome in disclosed mode among the embodiment 3 of JP11-1423A.More specifically, soybean lecithin, linoleic acid and dl-alpha-tocopherol are mixed equably with 1,3 butylene glycol, and to wherein adding purified water.The mixture that obtains is handled with French press (French press), thus preparation liposome dispersion (linoleic acid content: 0.5% or 1.0%).Based on the gross weight of liposome dispersion, for the preparation of the amount of each component be such, soybean lecithin content is 4 quality %, dl-alpha-tocopherol content is 0.05 quality %, and the content of 1,3 butylene glycol is 4 quality %.
Then, according to the prescription shown in the following table 1, component is mixed to prepare compositions (embodiment and comparative example)." other component " in the table 1 is identical in whole embodiment.The detail of " other component " provides in table 2.The numerical value of each component shows their amount (quality %) in the table 1 and 2.
Comparative example 1 shows such situation, wherein only uses L-cystine and L-threonine, and does not add tocopherol and phytic acid.Comparative example 2 shows such situation, wherein uses known oil-soluble Radix Glycyrrhizae extract (licorice extract) with antioxygenic property to replace tocopherol or phytic acid.
In addition, allow after production compositions was left standstill 2 months at 40 ℃.Then, with linoleic amount in each compositions quantitatively to check linoleic stability in each compositions.Linoleic quantitative assay is to be undertaken by high performance liquid chromatography (1100 series are produced by Agilent).Linoleic residual ratio is based on that the quantized value of application of mixture theory value after place calculate.Be estimated as follows at the linoleic acid residue ratio of 40 ℃ of placements after 2 months: the compositions with the linoleic acid residue ratio more than 95%: A; More than 90% and less than 95%:B; Less than 90%:C.Also show the result in the table 1.
Table 1
Table 2
Table 1 shows, the poor stability of linoleic acid in the compositions that contains the oil-soluble Radix Glycyrrhizae extract (comparative example 2).Find that also in the compositions that contains tocopherol separately, those that contain the dl-alpha-tocopherol acetate have the higher linoleic effect of stablizing than those that contain natural Vitamin E or Delta-Tocopherol.Find also that in addition the compositions that comprises L-cystine and L-threonine and tocopherol has the higher linoleic effect of stablizing than those that contain independent tocopherol.
The formulation example of the present composition is as follows." % " expression " quality % ", unless otherwise prescribed.The whole components except liposome that contain in the liposome dispersion are included in the continuous phase.
Table 3
Formulation example 1: elite
Group component (%)
Amount to 100
Table 4
Formulation example 2: emulsion
Group component (%)
Amount to 100
Table 5
Formulation example 3: emulsifiable paste
Group component (%)
Amount to 100
Claims (8)
1. component (A) and the component (B) shown in below compositions, described compositions comprise, described component (B) is dispersed in the continuous phase that contains described component (A):
(A) be selected from least one member in the group of being formed by tocopherol and phytic acid; With
(B) contain the liposome of polyunsaturated fatty acid or derivatives thereof.
2. compositions according to claim 1, wherein said tocopherol is at least one member who is selected from the group of being made up of alpha-tocopherol, betatocopherol, Gamma-Tocopherol, Delta-Tocopherol, dl-alpha-tocopherol acetate, dl-alpha-tocopherol and d-alpha-tocopherol acetate.
3. compositions according to claim 1 and 2, wherein said polyunsaturated fatty acid has 18 to 22 carbon atoms.
4. according to each described compositions in the claim 1 to 3, wherein said continuous phase contains phytic acid at least.
5. according to each described compositions in the claim 1 to 4, wherein said continuous phase contains Delta-Tocopherol at least.
6. according to each described compositions in the claim 1 to 5, wherein said continuous phase also contains at least one member who is selected from the group of being made up of L-cystine and L-threonine.
7. according to each described compositions in the claim 1 to 6, wherein said liposome also contains at least one member who is selected from the group of being made up of tocopherol and phytic acid.
8. according to each described compositions in the claim 1 to 7, described compositions is topical composition.
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| JP2011-015331 | 2011-01-27 | ||
| JP2011015331 | 2011-01-27 | ||
| PCT/JP2012/051751 WO2012102364A1 (en) | 2011-01-27 | 2012-01-27 | Composition containing polyunsaturated fatty acid |
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| CN103338746B CN103338746B (en) | 2015-12-23 |
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| US (1) | US8940312B2 (en) |
| EP (1) | EP2668939B1 (en) |
| JP (2) | JP6137836B2 (en) |
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| CN (1) | CN103338746B (en) |
| ES (1) | ES2804029T3 (en) |
| HK (1) | HK1185806A1 (en) |
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| CN116194082A (en) * | 2020-06-15 | 2023-05-30 | 犹他大学研究基金会 | Retinal bioavailability of synthetic ultralong chain polyunsaturated fatty acids |
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| JP6169240B1 (en) * | 2016-10-28 | 2017-07-26 | サンスター株式会社 | Linoleic acid-containing composition |
| WO2018108976A1 (en) * | 2016-12-13 | 2018-06-21 | Dsm Ip Assets B.V. | Pufa salt formulations (ii) |
| US10914810B2 (en) | 2018-05-17 | 2021-02-09 | Navico Holding As | Marine electronic device for presentment of nautical charts and sonar images |
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| JP6367399B2 (en) | 2018-08-01 |
| CN103338746B (en) | 2015-12-23 |
| ES2804029T3 (en) | 2021-02-02 |
| TWI580438B (en) | 2017-05-01 |
| US20130287827A1 (en) | 2013-10-31 |
| US8940312B2 (en) | 2015-01-27 |
| JP2017114895A (en) | 2017-06-29 |
| JPWO2012102364A1 (en) | 2014-06-30 |
| EP2668939A1 (en) | 2013-12-04 |
| KR101771063B1 (en) | 2017-08-24 |
| EP2668939A4 (en) | 2014-06-25 |
| JP6137836B2 (en) | 2017-05-31 |
| HK1185806A1 (en) | 2014-02-28 |
| TW201244747A (en) | 2012-11-16 |
| EP2668939B1 (en) | 2020-06-17 |
| WO2012102364A1 (en) | 2012-08-02 |
| KR20140012652A (en) | 2014-02-03 |
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